New insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent.
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ABSTRACT:
SUBMITTER: Zhu W
PROVIDER: S-EPMC4068539 | biostudies-literature | 2014 Jul
REPOSITORIES: biostudies-literature
Publications
New insights into the bacterial RNA polymerase inhibitor CBR703 as a starting point for optimization as an anti-infective agent.
Zhu Weixing W Haupenthal Jörg J Groh Matthias M Fountain Michelle M Hartmann Rolf W RW
Antimicrobial agents and chemotherapy 20140512 7
CBR703 was reported to inhibit bacterial RNA polymerase (RNAP) and biofilm formation, considering it to be a good candidate for further optimization. While synthesized derivatives of CBR703 did not result in more-active RNAP inhibitors, we observed promising antibacterial activities. These again correlated with a significant cytotoxicity toward mammalian cells. Furthermore, we suspect the promising effects on biofilm formation to be artifacts. Consequently, this class of compounds can be conside ...[more]
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